Literature DB >> 18442904

Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda6-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones: Part 4. Optimization of DMPK properties.

Maria V Sergeeva1, Yuefen Zhou, Darian M Bartkowski, Thomas G Nolan, Daniel A Norris, Ellen Okamoto, Leo Kirkovsky, Ruhi Kamran, Laurie A Lebrun, Mei Tsan, Rupal Patel, Amit M Shah, Matthew Lardy, Alberto Gobbi, Lian-Sheng Li, Jingjing Zhao, Thomas Bertolini, Nebojsa Stankovic, Zhongxiang Sun, Douglas E Murphy, Stephen E Webber, Peter S Dragovich.   

Abstract

5-Hydroxy-3(2H)-pyridazinone derivatives were investigated as potent inhibitors of genotype 1 HCV NS5B polymerase focusing on the optimization of their drug metabolism and pharmacokinetics (DMPK) profiles. This investigation led to the discovery of potent inhibitors with improved DMPK properties.

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Year:  2008        PMID: 18442904     DOI: 10.1016/j.bmcl.2008.04.005

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  QSAR study of C allosteric binding site of HCV NS5B polymerase inhibitors by support vector machine.

Authors:  Eslam Pourbasheer; Siavash Riahi; Mohammad Reza Ganjali; Parviz Norouzi
Journal:  Mol Divers       Date:  2010-10-08       Impact factor: 2.943

  1 in total

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